ofatumumab Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
human origin 4951 679818-59-8

Description:

MoleculeDescription

Synonyms:

  • ofatumumab
  • arzerra
  • GSK1841157
  • HuMax-CD20
  • 2F2
Ofatumumab is a human monoclonal antibody (IgG1) that binds specifically to a distinct epitope encompassing both the small and large extracellular loops of the CD20 molecule. The CD20 molecule is a transmembrane phosphoprotein expressed on B lymphocytes from the pre-B to mature B lymphocyte stage and on B cell tumours. The binding of ofatumumab to the membrane-proximal epitope of the CD20 molecule induces recruitment and activation of the complement pathway at the cell surface, leading to complement dependent cytotoxicity and resultant lysis of tumour cells. Ofatumumab has been shown to induce appreciable lysis of cells with high expression levels of complement defence molecules.
  • Molecular weight:
  • Formula:
  • CLOGP:
  • LIPINSKI: None
  • HAC: None
  • HDO: None
  • TPSA:
  • ALOGS:
  • ROTB: None

Drug dosage:

None

ADMET properties:

None

Approvals:

DateAgencyCompanyOrphan
April 19, 2010 EMA Novartis Europharm Ltd
Oct. 26, 2009 FDA GLAXO GRP LTD

FDA Adverse Event Reporting System (Female)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Febrile neutropenia 202.34 30.67 86 1495 94541 46589940
Progressive multifocal leukoencephalopathy 63.54 30.67 21 1560 11325 46673156
Pyrexia 62.08 30.67 67 1514 348735 46335746
Pneumonia 59.59 30.67 68 1513 376252 46308229
Chronic lymphocytic leukaemia 55.60 30.67 14 1567 2886 46681595
Neutropenic sepsis 46.53 30.67 17 1564 12307 46672174
Neutropenia 35.38 30.67 33 1548 143171 46541310
Chills 33.58 30.67 27 1554 96005 46588476
Hemianopia 31.00 30.67 7 1574 906 46683575

FDA Adverse Event Reporting System (Male)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Febrile neutropenia 218.23 31.29 132 2745 106561 29843040
Pneumonia 148.83 31.29 170 2707 334136 29615465
Neutropenic sepsis 112.53 31.29 42 2835 11367 29938234
Chronic lymphocytic leukaemia 109.77 31.29 33 2844 4595 29945006
Pyrexia 80.25 31.29 118 2759 294371 29655230
Infusion related reaction 54.95 31.29 39 2838 40525 29909076
Second primary malignancy 53.98 31.29 21 2856 6335 29943266
Disease progression 53.61 31.29 51 2826 79823 29869778
Tumour lysis syndrome 45.53 31.29 23 2854 12862 29936739
Neutropenia 44.44 31.29 58 2819 128482 29821119
Hypercalcaemia 34.73 31.29 19 2858 12476 29937125
Lower respiratory tract infection 32.30 31.29 24 2853 26690 29922911

Pharmacologic Action:

SourceCodeDescription
ATC L01XC10 ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
ANTINEOPLASTIC AGENTS
OTHER ANTINEOPLASTIC AGENTS
Monoclonal antibodies
FDA MoA N0000175078 CD20-directed Antibody Interactions
FDA EPC N0000175657 CD20-directed Cytolytic Antibody
MeSH PA D000970 Antineoplastic Agents

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Chronic lymphoid leukemia, disease indication 92814006
Relapsing multiple sclerosis indication 230372003

Acid dissociation constants calculated using MoKa v3.0.0

None

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
B-lymphocyte antigen CD20 Surface antigen ANTIBODY BINDING Kd 9.92 IUPHAR DRUG LABEL

External reference:

IDSource
D09314 KEGG_DRUG
4029460 VUID
N0000180305 NUI
4029460 VANDF
C4732982 UMLSCUI
CHEMBL1201836 ChEMBL_ID
8254 PUBCHEM_CID
DB06650 DRUGBANK_ID
C527517 MESH_SUPPLEMENTAL_RECORD_UI
6778 IUPHAR_LIGAND_ID
8606 INN_ID
M95KG522R0 UNII
712566 RXNORM
168892 MMSL
26825 MMSL
d07509 MMSL
013301 NDDF
444607009 SNOMEDCT_US
444609007 SNOMEDCT_US
895672000 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
ARZERRA HUMAN PRESCRIPTION DRUG LABEL 1 0078-0669 INJECTION, SOLUTION 20 mg INTRAVENOUS BLA 26 sections
ARZERRA HUMAN PRESCRIPTION DRUG LABEL 1 0078-0690 INJECTION, SOLUTION 20 mg INTRAVENOUS BLA 26 sections
KESIMPTA HUMAN PRESCRIPTION DRUG LABEL 1 0078-1007 INJECTION, SOLUTION 20 mg SUBCUTANEOUS BLA 30 sections